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2oiq

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[[Image:2oiq.gif|left|200px]]<br /><applet load="2oiq" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2oiq.gif|left|200px]]
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caption="2oiq, resolution 2.07&Aring;" />
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'''Crystal Structure of chicken c-Src kinase domain in complex with the cancer drug imatinib.'''<br />
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{{Structure
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|PDB= 2oiq |SIZE=350|CAPTION= <scene name='initialview01'>2oiq</scene>, resolution 2.07&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=STI:4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE'>STI</scene> and <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2]
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|GENE= SRC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9031 Gallus gallus])
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}}
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'''Crystal Structure of chicken c-Src kinase domain in complex with the cancer drug imatinib.'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2OIQ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus] with <scene name='pdbligand=STI:'>STI</scene> and <scene name='pdbligand=GOL:'>GOL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OIQ OCA].
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2OIQ is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OIQ OCA].
==Reference==
==Reference==
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c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty., Seeliger MA, Nagar B, Frank F, Cao X, Henderson MN, Kuriyan J, Structure. 2007 Mar;15(3):299-311. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17355866 17355866]
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c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty., Seeliger MA, Nagar B, Frank F, Cao X, Henderson MN, Kuriyan J, Structure. 2007 Mar;15(3):299-311. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17355866 17355866]
[[Category: Gallus gallus]]
[[Category: Gallus gallus]]
[[Category: Non-specific protein-tyrosine kinase]]
[[Category: Non-specific protein-tyrosine kinase]]
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[[Category: src]]
[[Category: src]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:19:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:00:14 2008''

Revision as of 16:00, 20 March 2008

Image:2oiq.gif


PDB ID 2oiq

Drag the structure with the mouse to rotate
, resolution 2.07Å
Ligands: and
Gene: SRC (Gallus gallus)
Activity: Non-specific protein-tyrosine kinase, with EC number 2.7.10.2
Coordinates: save as pdb, mmCIF, xml



Crystal Structure of chicken c-Src kinase domain in complex with the cancer drug imatinib.


Overview

The cancer drug imatinib inhibits the tyrosine kinases c-Abl, c-Kit, and the PDGF receptor. Imatinib is less effective against c-Src, which is difficult to understand because residues interacting with imatinib in crystal structures of Abl and c-Kit are conserved in c-Src. The crystal structure of the c-Src kinase domain in complex with imatinib closely resembles that of Abl*imatinib and c-Kit*imatinib, and differs significantly from the inactive "Src/CDK" conformation of the Src family kinases. Attempts to increase the affinity of c-Src for imatinib by swapping residues with the corresponding residues in Abl have not been successful, suggesting that the thermodynamic penalty for adoption of the imatinib-binding conformation by c-Src is distributed over a broad region of the structure. Two mutations that are expected to destabilize the inactive Src/CDK conformation increase drug sensitivity 15-fold, suggesting that the free-energy balance between different inactive states is a key to imatinib binding.

About this Structure

2OIQ is a Single protein structure of sequence from Gallus gallus. Full crystallographic information is available from OCA.

Reference

c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty., Seeliger MA, Nagar B, Frank F, Cao X, Henderson MN, Kuriyan J, Structure. 2007 Mar;15(3):299-311. PMID:17355866

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